Acylated amine compounds which are useful fungicigal agents
    1.
    发明授权
    Acylated amine compounds which are useful fungicigal agents 失效
    有用的真菌药剂的胺化合物

    公开(公告)号:US5064861A

    公开(公告)日:1991-11-12

    申请号:US454685

    申请日:1989-12-21

    摘要: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of Ar-O- and aryl, polyaryl and condensed polyaryl unsubstituted or substituted and heterocycle unsubstituted or substituted, Ar is aryl of 6 to 14 carbon atoms unsubstituted or substituted, heteroaryl unsubstituted or substituted and heterocyclic unsubstituted or substituted, W is selected from the group comsisting of --(CH.sub.2).sub.n.sbsb.1 --or --(CH.sub.2).sub.n.sbsb.2 --NY--(CH.sub.2).sub.n.sbsb.3, n.sub.1, n.sub.2 and n.sub.3 are individually integers from 2 to 6, Y is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms, aryl of 6 to 12 carbon atoms and aralkyl of 7 to 14 carbon atoms unsubstituted or substituted, --COOAlk and --COR.sub.2, Alk is alkyl of 1 to 12 carbon atoms, R.sub.2 is selected from the group consisting of alkyl of 1 to 12 carbon atoms, alkenyl and alkynyl of 2 to 12 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms unsubstituted or substituted and heterocyclic unsubstituted or substituted, Z is selected from the group consisting of hydrogen, ##STR2## R.sub.2 is alkyl of 1 to 12 carbon atoms or aralkyl of 7 to 18 carbon atoms, Alk' is alkyl of 1 to 12 carbon atoms, ArAlk is aralkyl of 7 to 18 carbon atoms, R.sub.2 ' is R.sub.2, R.sub.3 and R.sub.3 ' are selected from the group consisting of aryl substituted or unsubstituted, heteroaryl substituted or unsubstituted, heterocyclic unsubstituted or substituted and R.sub.1 with the proviso that Z is not hydrogen when W is --(CH.sub.2).sub.3 --and R.sub.1 is 2,4-dichlorophenoxy and their non-toxic, pharmaceutically acceptable acid addition salts having fungicidal activity.

    摘要翻译: 选自下式的化合物的化合物其中R 1选自Ar-O-和芳基,聚芳基和未取代或取代的缩合聚芳基,未取代或取代的杂环,Ar是 未取代或未取代的未取代或未取代的杂芳基,未取代或取代的杂芳基,W选自 - (CH 2)n1 - 或 - (CH 2)n 2 -YH-(CH 2)n3,n1,n2 和n3各自为2至6的整数,Y选自氢,1至12个碳原子的烷基,6至12个碳原子的芳基和未被取代或取代的7-14个碳原子的芳烷基,-COOAlk和 -COR 2,Alk为1〜12个碳原子的烷基,R2选自1〜12个碳原子的烷基,2〜12个碳原子的烯基和炔基,6〜14个碳原子的芳基,7个芳烷基 至18个碳原子未被取代或取代和杂合 Z取代或未取代的Z选自氢,-COCH 2 R 3,R 2是1至12个碳原子的烷基或7至18个碳原子的芳烷基,Alk'是1至12个碳的烷基 原子,ArAlk是7至18个碳原子的芳烷基,R2'是R2,R3和R3'选自芳基取代或未取代的杂芳基取代或未取代的杂环,未取代或取代的杂环,R1是条件是Z是 当W是 - (CH 2)3 - 且R 1是2,4-二氯苯氧基时,它们不是氢,它们是具有杀真菌活性的无毒的药学上可接受的酸加成盐。

    Insecticidal benzofuran derivatives
    2.
    发明授权
    Insecticidal benzofuran derivatives 失效
    杀虫剂苯唑嘌呤衍生物

    公开(公告)号:US5182295A

    公开(公告)日:1993-01-26

    申请号:US770986

    申请日:1991-10-01

    摘要: A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl, alkenyl and alkynyl of up to 8 carbon atoms, optionally substituted cycloalkyl or cycloalkenyl of up to 8 carbon atoms, optionally substituted aryl of 6 to 18 carbon atoms, optionally substituted aralkyl of 7 to 24 carbon atoms, optionally substituted benzoyl and optionally substituted heterocycle, the optional substituents being at least one member of the group consisting of halogen, phenoxy, thiazolyl, alkyl and alkoxy of 1 to 6 carbon atoms and haloalkyl, Alk.sub.1 and Alk.sub.2 are individually optionally substituted alkyl of 1 to 8 carbon atoms, X is --O-- or --S-- and R' is hydrogen or halogen in any position on the phenyl and the geometry of the double bond is E or Z or a mixture of E and Z and having useful pesticidal properties.

    摘要翻译: 下式的化合物其中R选自氢,任选取代的烷基,链烯基和至多8个碳原子的炔基,任选取代的环烷基或至多8个碳原子的环烯基,任选取代的芳基 6至18个碳原子,任选取代的7至24个碳原子的芳烷基,任选取代的苯甲酰基和任选取代的杂环,任选的取代基是1至6个卤素,苯氧基,噻唑基,烷基和烷氧基中的至少一个成员 碳原子和卤代烷基,Alk1和Alk2分别是1至8个碳原子的任意取代的烷基,X是-O-或-S-,R'是氢或卤素在苯基上的任何位置,双键的几何形状是 E或Z或E和Z的混合物,并具有有用的杀虫性质。

    Polyunsaturated compounds, method for preparing same and compositions containing the same
    3.
    发明授权
    Polyunsaturated compounds, method for preparing same and compositions containing the same 失效
    多不饱和化合物,其制备方法和含有它们的组合物

    公开(公告)号:US08420610B2

    公开(公告)日:2013-04-16

    申请号:US12086625

    申请日:2006-12-14

    摘要: The invention concerns novel polyunsaturated compounds of formula (I) wherein: R1 represents a R′1, -A-R′1 group, R′1 being selected from —COOH, —COOR3, —CONH2, —CONHR3, —CONR3 R4, —CHO, —CH2OH, —CH2OR5, and A represents a C2-C16 alkylene, alkenylene or alkynylene; R2 represents: an optionally substituted aryl group or an optionally substituted heteroaryl group; a sugar residue or, a fatty acid residue optionally branched and/or substituted preferably at the chain terminus and particularly by hydroxy, acetoxy radical or by an optionally protected amino radical; a —OC —(CH2)n CO-tocopheryl (alpha, beta or gamma or delta) group, with 2 $m(F) n $m(F) 10; a —R′2—O—R6 group, wherein R′2 is an optionally substituted arylene group or an optionally substituted heteroarylene group, and R6 represents a hydrogen atom, a straight or branched optionally substituted C 1-C 16 alkyl, a straight or branched optionally substituted C2-C16 alkenyl, or a straight or branched C2-C16 alkynyl group, an optionally substituted tocopheryl radical or the like, an amino acid residue, or a sugar residue. The invention also concerns the compositions, in particular cosmetic and/or dermatological compositions containing at least one compound of formula (I) as well as their use as whitening and/or depigmenting agent, and the cosmetic method using said compositions.

    摘要翻译: 本发明涉及式(I)的新型多不饱和化合物,其中:R1表示R'1,-AR'1基团,R'1选自-COOH,-COOR3,-CONH2,-CONHR3,-CONR3R4,-CHO ,-CH 2 OH,-CH 2 OR 5,A表示C 2 -C 16亚烷基,亚烯基或亚炔基; R2表示:任选取代的芳基或任选取代的杂芳基; 糖残基或脂肪酸残基,优选在链末端,特别是通过羟基,乙酰氧基或任选被保护的氨基部分支化和/或取代; a -OC-(CH 2)n CO-生育酚(α,β或γ或δ)组,其中2 $ m(F)n $ m(F)10; -R'2-O-R6基团,其中R'2是任选取代的亚芳基或任选取代的亚杂芳基,R 6表示氢原子,直链或支链任选取代的C 1 -C 16烷基,直链 或支链任选取代的C 2 -C 16烯基,或直链或支链C 2 -C 16炔基,任选取代的生育酚基等,氨基酸残基或糖残基。 本发明还涉及组合物,特别是包含至少一种式(I)化合物的化妆品和/或皮肤病学组合物,以及它们作为增白剂和/或脱色素剂的用途,以及使用所述组合物的美容方法。

    Alpha-methylene-6-styryl-acrylic acid derivatives
    4.
    发明授权
    Alpha-methylene-6-styryl-acrylic acid derivatives 失效
    α-亚甲基-6-苯乙烯基 - 丙烯酸衍生物

    公开(公告)号:US5310746A

    公开(公告)日:1994-05-10

    申请号:US981071

    申请日:1992-11-24

    摘要: All possible stereoisomer forms and mixtures of a compound of the formula ##STR1## wherein X is a halogen, R.sub.2 and R.sub.3 are individually selected from the group consisting of alkyl and cycloalkyl of up to 8 carbon atoms optionally substituted with at least one halogen, R.sub.1 is selected from the group consisting of alkyl, alkenyl, alkynyl and cycloalkyl of up to 12 carbon atoms optionally substituted with at least one halogen, aryl and heteroaryl of 5 to 6 ring members optionally substituted with at least one member of the group consisting of halogen, alkyl, alkenyl, alkynyl and cycloalkyl of up to 8 carbon atoms optionally substituted with at least one member of the group consisting of --NO.sub.2, --NH.sub.2, --CN, --OR', --SR", --SOR", --SO.sub.2 R", --NR"'.sub.2, --Ar, OAr.sub.1 and SAr.sub.2, R', R" and R"' are individually selected from the group consisting of alkyl, alkenyl, alkynyl and cycloalkyl of up to 12 carbon atoms optionally substituted by at least one halogen, Ar, Ar.sub.1 and Ar.sub.2 are aryl or heteroaryl of up to 14 carbon atoms optionally substituted with at least one member of the group consisting of halogen and alkyl, alkenyl, alkynyl and cycloalkyl of up to 8 carbon atoms optionally substituted by at least one member of the group consisting of halogen, --NO.sub.2, --NH.sub.2, --CN, --OR', --SR", --SOR", --SO.sub.2 R" and --NR"'.sub.2 and R', R" and R"' have the above definitions and their preparations and novel intermediates useful as pesticides.

    摘要翻译: 所有可能的立体异构体形式和式I化合物的混合物,其中X是卤素,R 2和R 3分别选自任选被至少一个卤素取代的至多8个碳原子的烷基和环烷基, R 1选自由至多12个碳原子的烷基,烯基,炔基和环烷基组成的组,其任选被至少一个5至6个环成员的卤素,芳基和杂芳基取代,任选被至少一个成员 卤素,烷基,烯基,炔基和至多8个碳原子的环烷基,任选被至少一个由-NO 2,-NH 2,-CN,-OR',-SR“,-SOR”, -SO 2 R“,-NR”'2,-Ar,OAr 1和SAr 2,R',R“和R”'分别选自至多12个碳的烷基,烯基,炔基和环烷基 任选被至少一个卤素取代的原子,Ar,Ar 1和Ar 2是至多1个的芳基或杂芳基 4个碳原子,任选被至少一个由卤素和至多8个碳原子的烷基,烯基,炔基和环烷基组成的组取代,任选被至少一个卤素,-NO 2,-NH 2, -CN,-OR',-SR“,-SOR”,-SO 2 R“和-NR”'2和R',R“和R”'具有上述定义及其制备和新型中间体 作为农药有用

    UNSATURATED FATTY AMINO ACID DERIVATIVES AND USE THEREOF IN DERMAL COSMETOLOGY
    6.
    发明申请
    UNSATURATED FATTY AMINO ACID DERIVATIVES AND USE THEREOF IN DERMAL COSMETOLOGY 审中-公开
    不饱和脂肪氨基酸衍生物及其在真菌学中的应用

    公开(公告)号:US20100240754A1

    公开(公告)日:2010-09-23

    申请号:US12523231

    申请日:2008-01-16

    摘要: The present invention relates to drugs consisting of unsaturated fatty amino-acid derivatives of the general formula (I), and to their pharmaceutically acceptable acid addition salts, in which: X is oxygen or NH, Rn are independently hydrogen or a (C1-C6)alkyl optionally substituted by halogen; R1 is hydrogen, fluorine, chlorine or bromine, or a CF3 or CHF2 or a (C1-C6)alkyl, (C1-C6)alkenyl or (C1-C6)alkynyl, optionally substituted by one or more halogen atoms; R is hydrogen or a (C1-C6)alkyl or (C3-C6)cycloalkyl optionally substituted by one or more halogen atoms; Ra and Rb are independently hydrogen (C1-C6)alkyl or (C1-C6)acyl, and Ra and Rb a hydrocarbonated cycle containing 4 to 6 carbon atoms; and n is an integer between 2 and 14.

    摘要翻译: 本发明涉及由通式(I)的不饱和脂肪氨基酸衍生物及其药学上可接受的酸加成盐组成的药物,其中:X为氧或NH,R n独立地为氢或(C 1 -C 6 )烷基任选被卤素取代; R 1是任选被一个或多个卤素原子取代的氢,氟,氯或溴,或CF 3或CHF 2或(C 1 -C 6)烷基,(C 1 -C 6)烯基或(C 1 -C 6) R是氢或任选被一个或多个卤素原子取代的(C 1 -C 6)烷基或(C 3 -C 6)环烷基; Ra和Rb独立地是氢(C1-C6)烷基或(C1-C6)酰基,Ra和Rb是含有4-6个碳原子的烃基; n为2〜14的整数。

    .alpha.-methylene-5-thiazolacetic acid esters
    8.
    发明授权
    .alpha.-methylene-5-thiazolacetic acid esters 失效
    (ALPHA)-METHYLENE-5-THIAZOLAC酸性酯

    公开(公告)号:US5210093A

    公开(公告)日:1993-05-11

    申请号:US851926

    申请日:1992-03-16

    摘要: A compound of the formula ##STR1## wherein Ar is phenyl optionally substituted with at least one member of the group consisting of halogen, methylenedioxy, phenyl, phenoxy, --CF.sub.3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, Z is selected from the group consisting of hydrogen, chlorine, --CF.sub.3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, R.sub.1 and R.sub.2 are individually alkyl of 1 to 6 carbon atoms and the exocyclic double bonds independently have (E) or (Z) geometry having fungicidal activity and a process for their preparation.

    摘要翻译: 式I的化合物,其中Ar是任选被至少一个由卤素,亚甲二氧基,苯基,苯氧基,-CF 3和1-6个碳原子的烷基,烷氧基和烷硫基取代的基团,Z是 选自氢,氯,-CF 3和具有1至6个碳原子的烷基,烷氧基和烷硫基,R 1和R 2分别是1至6个碳原子的烷基,并且环外双键独立地具有(E)或(Z )几何具有杀真菌活性及其制备方法。

    Process for preparation of thiazolylalkoxy acrylates
    9.
    发明授权
    Process for preparation of thiazolylalkoxy acrylates 失效
    制备三唑烷基丙烯酸酯的方法

    公开(公告)号:US5194622A

    公开(公告)日:1993-03-16

    申请号:US793862

    申请日:1991-11-18

    CPC分类号: C07F9/5456 C07D277/30

    摘要: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, halogen, --CF.sub.3, alkyl, alkoxy and alkylthio of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, --SO.sub.2 alk and alk is alkyl of 1 to 8 carbon atoms, optionally substituted aryl, aryloxy and arylthio of 6 to 18 carbon atoms and optionally substituted heteroaryl, heteroaryloxy and heterocyclic of 5 to 6 ring members, R.sub.3 is selected from the group consisting of alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 18 carbon atoms and alkoxyalkoxyalkyl of 3 to 14 carbon atoms, X is selected from the group consisting of --O--, --S-- and --NR.sub.4 --, R.sub.4 is selected from the group consisting of hydrogen, alkyl, alkenyl and alkynyl of up to 8 carbon atoms, --SO.sub.2 alkyl, --SO.sub.2 alkenyl and --SO.sub.2 alkynyl of up to 8 carbon atoms and optionally substituted aryl and --SO.sub.2 aryl of 6 to 18 carbon atoms, the double bond between the heterocycle of 5 member ring and the aromatic nucleus is of E and/or Z geometry comprising reacting a halide of the formula ##STR2## wherein R.sub.3 is as defined above and Hal is hydrogen with a compound of the formula ##STR3## wherein X, R.sub.1 and R.sub.2 have the above definitions in the presence of a base to obtain the corresponding product of formula I in the form of a mixture of isomers and optionally separating the isomers and novel intermediates of formula II.

    摘要翻译: 制备式I化合物的方法,其中R 1和R 2分别选自氢,卤素,-CF 3,具有1至8个碳原子的烷基,烷氧基和烷硫基,烯基和炔基 2至8个碳原子,-SO 2alk和alk是1至8个碳原子的烷基,任选取代的芳基,6至18个碳原子的芳氧基和芳硫基以及任选取代的杂芳基,杂芳氧基和5至6个环成员的杂环, 由1-8个碳原子的烷基,2至8个碳原子的烯基和炔基,6至18个碳原子的芳基和3至14个碳原子的烷氧基烷氧基烷基组成的组,X选自-O- ,-S-和-NR4-,R4选自具有至多8个碳原子的氢,烷基,烯基和炔基,-SO 2烷基,-SO 2链烯基和至多8个碳原子的-SO 2炔基, 取代的芳基和6至18个碳原子的-SO 2芳基,双键 e是5元环的杂环,并且芳香核具有E和/或Z几何形状,包括使式II的卤化物其中R 3如上所定义,Hal是氢的式IIIa化合物与式 其中X,R 1和R 2在碱的存在下具有上述定义,以获得异构体混合物形式的相应的式I产物,并任选分离式II的异构体和新型中间体。

    .alpha.-methylene-5-thiazolacetic acid esters
    10.
    发明授权
    .alpha.-methylene-5-thiazolacetic acid esters 失效
    α-亚甲基-5-噻唑乙酸酯

    公开(公告)号:US5508414A

    公开(公告)日:1996-04-16

    申请号:US342337

    申请日:1994-11-18

    摘要: A compound of the formula ##STR1## wherein Ar is phenyl optionally substituted with at least one member of the group consisting of halogen, methylenedioxy, phenyl, phenoxy, --CF.sub.3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, Z is selected from the group consisting of hydrogen, chlorine, --CF.sub.3 and alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, R.sub.1 and R.sub.2 are individually alkyl of 1 to 6 carbon atoms and the exocyclic double bonds independently have (E) or (Z) geometry having fungicidal activity and a process for their preparation.

    摘要翻译: 式I的化合物,其中Ar是任选被至少一个由卤素,亚甲二氧基,苯基,苯氧基,-CF 3和1-6个碳原子的烷基,烷氧基和烷硫基取代的基团,Z是 选自氢,氯,-CF 3和具有1至6个碳原子的烷基,烷氧基和烷硫基,R 1和R 2分别是1至6个碳原子的烷基,并且环外双键独立地具有(E)或(Z )几何具有杀真菌活性及其制备方法。